Derm drugs Flashcards

Question

purpose of Becaplermin

Answer 1

Platelet derived growth factor that promotes cell proliferation and angiogenesis only approved for treatment of chronic diabetic foot ulcers black box warning for malignancy

Answer 2

no! does not significantly improve epithelialization

Answer 3

general principles: wounds should be kept moist , and should not be exposed to air as done historically – occluded wounds heal 40% faster and have less scarring – wounds are exposed to their own fluid, a mix of metalloproteases and cytokines • consensus opinion on choices: – hydrogels for debridement stage – foam and low adherence dressings for the granulation stage – hydrocolloid and low adherence dressings for epithelialization stage

Answer 4

Topical antibacterial agent ``` peptide antibiotic, inhibits bacterial cell wall synthesis • active against gram positive organisms, also active against most anaerobic cocci, neisseriae , tetanus bacilli, diphtheria bacilli • often causes allergic contact dermatitis, and rarely immunologic allergic contact urticaria • poorly absorbed through the skin, so systemic toxicity is rare ```

Answer 5

Topical antibacterial agent ``` aminoglycoside antibiotic, binds to 30S ribosomal subunit to inhibit protein synthesis • active against gram negative organisms • o ften causes allergic contact dermatitis, and cross sensitization to other aminoglycosides can occur • poorly absorbed through the skin, so systemic detection is rare ```

Answer 6

``` peptide antibiotic, binds to phosphor lipids to alter permeability and damage bacterial cytoplasmic membrane • effective against gram negative organisms, including P. aeruginosa, E. coli, Enterobacter , and Klebsiella • rarely causes allergic reaction ```

Answer 7

topical imidazoles , block ergosterol synthesis, have a wide range of activity against dermatophytes and yeasts – miconazole … topical application as a cream or lotion; vaginal cream or suppositories for use in vulvovaginal candidiasis – clotrimazole … topical application to the skin as a cream or lotion; vaginal cream and tablets for use in vulvovaginal candidiasis – efinaconazole … onychomycosis treatment, given for 48 weeks, complete cure in ~15 % 18% – ketoconazole … cream for topical treatment of dermatophytosis and candidiasis, shampoo or foam for seborrheic dermatitis

Answer 8

Topical antifungal agent prescription synthetic broad spectrum topical antimycotic agent, disrupts macromolecular synthesis – activity against dermatophytes, Candida and Malassezia – low incidence of adverse reactions and contact dermatitis

Answer 9

Topical antifungal agent allylamine , selectively inhibits squalene epoxidase, a key enzyme for the synthesis of ergosterol – highly active against dermatophytes but less active against yeasts – cream can cause local irritation, avoid contact with mucous membranes

Answer 10

synthetic antifungal compound, mechanism uncertain but distorts hyphae/stunts mycelial growth – effective topically against various dermatophyte and malessezia infections but not Candida – generally well tolerated and rarely causes irritation or allergic contact dermatitis

Answer 11

Topical antifungal agent binds to fungal sterols, alters membrane permeability – limited to topical treatment of cutaneous and mucosal candida infections (hold in mouth before swallowing) because of its narrow spectrum and negligible absorption from the gastrointestinal tract following oral administration – non irritating topically; mild nausea and diarrhea if swallowed

Answer 12

Topical antifungal agent binds to fungal sterols, alters membrane permeability – limited to topical treatment of cutaneous candida infections – well tolerated, but may cause a temporary yellow staining of the skin

Answer 13

``` synthetic guanine analog with inhibitory activity against herpes simplex types 1 and 2 – u sed for the treatment of recurrent orolabial herpes simplex virus infection (herpes labialis ) in immunocompetent adults – o intment, cream and buccal tablet formulations available ```

Answer 14

Skin moisturization dry skin can cause or exacerbate pruritus; thus, all patients with generalized symptoms should use gentle cleansers and apply emollients daily • Cool environment heat can worsen symptoms, so light weight clothing, air conditioned environments, and the use of lukewarm water during showers or baths may reduce symptoms; cooling lotions (calamine, those with menthol) can provide additional relief. • Avoidance of skin irritants wool clothing and cleansing products are among common irritants • Stress reduction psychological support and behavioral interventions that help patients to cope are important including holistic approaches such as meditation, acupuncture, and yoga. • Physical interventions Break the itch scratch cycle by occluding localized areas of pruritus with occlusive dressings

Answer 15

``` Tacrolimus 0.03% and 0.1% ointment Particularly useful in anogenital pruritus , may experience transient burning and stinging Pimecrolimus 1% cream ```

Answer 16

H1 antagonist 5% cream Avoid in children, 20 to 25 percent risk of sedation

Answer 17

TRPM8 agonist 0.025 to 0.1% cream Particularly useful in neuropathic itch , may experience initial transient burning

Answer 18

``` Pramoxine 1 to 2.5% found in a variety of OTC remedies along with hydrocortisone; e.g., useful for pruritus on face and that associated with CKD Lidocaine patch 5% Useful in neuropathic pruritus Eutectic mixture of lidocaine 2.5% and prilocaine 2.5% Useful in neuropathic pruritus ```

Answer 19

Use low potency on face, genitals and skin folds (class 7) elsewhere, generally start high potency to gain control and titrate downward for maintenance (class 1)

Answer 20

Activates TRPV1 (heat) channels topical sensation for pruitus substance derived from chili peppers that has been used for the treatment of chronic pain and pruritus • t he mechanism of action for capsaicin involves its ability to activate transient release potential vanilloid 1 (TRPV1), an ion channel in cutaneous nerve fibers • activation of TRPV1 stimulates neurons to release and eventually deplete certain neuropeptides, including substance P • c apsaicin also induces lasting desensitization of neurons to a variety of stimuli

Answer 21

known since ancient times for its anti inflammatory activities – a COX inhibitor – unripe fruits are natural sources • also found in many skin care products (e.g., for treatment of acne, dandruff) – causes epidermal cells to shed more readily ( keratolytic ), has antibacterial properties, and opens clogged pores – keratolytic effects caused by its ability to dissolve the intercellular cement; applied in more concentrated solutions (e.g., 6% in petrolatum) to calluses for 1 hr before washing away – treated areas are photosensitized, need protection from sun • prolonged use can cause salicylate toxicity, especially in children and those with reduced kidney or liver function

Answer 22

antidepressant ``` m irtazapine 7.5 to 15 mg at night Useful in nocturnal pruritus , may cause increased weight and appetite ```

Answer 23

paroxetine 10 to 40 mg per day Consider in psychiatric patients with pruritus and paraneoplastic pruritus fluvoxamine 25 to 150 mg per day Consider in psychiatric patients with pruritus and paraneoplastic pruritus sertraline 75 to 100 mg per day Useful in cholestatic pruritus

Answer 24

naltrexone 25 to 50 mg per day Useful in patients with cholestatic and CKD associated pruritus ; may cause nausea, vomiting and drowsiness; reverses analgesia and may precipitate acute withdrawal in patients receiving opioid analgesics

Answer 25

butorphanol 1 to 4 mg intranasally per day Useful in nocturnal and intractable pruritus ; may cause nausea and vomiting as well as drowsiness; may precipitate acute withdrawal in patients receiving opioid analgesics; some potential for abuse due to concomitant weak µ opioid receptor agonist activity

Answer 26

gabapentin 100 to 3600 mg per day useful in neuropathic pruritus , may cause drowsiness and weight gain; usually given in two to three divided daily doses; dose alteration for renal insufficiency may be needed pregabalin 150 to 300 mg per day

Answer 27

aprepitant 80 mg per day more commonly used to control nausea/vomiting of chemotherapy, but has shown benefits in patients with intractable pruritus (e.g., Sézary syndrome)

Answer 28

• brimonidine … α 2 adrenergic agonist applied as a topical gel , vasoconstricts by stimulating post synaptic vascular α 2 receptors. • oxymetazoline … mixed α 1A α 2 adrenergic agonist vasoconstrictor applied as a topical cream , approved 2017

Answer 29

naphazoline , tetrahydrozoline , phenylephrine and oxymetazoline … eye drops are all adrenergic receptor agonists

Answer 30

• malathion … topical agent, organophosphate cholinesterase inhibitor • permethrin … topical agent, binds to insect Na channels, blocks membrane repolarization • ivermectin … administered orally, binds to glutamate gated Cl channels in invertebrates, hyperpolarizes the nerve and muscle cells • lindane … topical agent, toxicity causes to be used only after other agents fail, disrupts GABAergic transmission in insects

Answer 31

Topical retinoids for acne ``` Once daily, at bedtime Creams: 0.025%, 0.0375%, 0.05%, 0.1% Polyolprepolymer 2 cream: 0.025% Gels: 0.01%, 0.025%, 0.05% Microsphere gels: 0.04%, 0.1% Polyolprepolymer 2 gel: 0.025% Gel (micronized): 0.05% Local skin irritation, dryness, and flaking; sun sensitivity NOTE: Atralin ® contains soluble fish proteins, use with caution in patients with known sensitivity or allergy to fish ```

Answer 32

topical retinoid for acne ``` Once daily, at bedtime Cream: 0.1% Gels: 0.1%, 0.3% Lotion: 0.1% Local skin irritation, dryness, and flaking; sun sensitivity ```

Answer 33

Topical retinoid for acne ``` Tazarotene Once daily, at bedtime Creams: 0.05%, 0.1% Gels: 0.05%, 0.1% Pregnancy category X; local skin irritation, dryness, and flaking; sun sensitivity ```

Answer 34

Topical antimicrobial for acne ``` Twice daily Multiple 2.5 to 10% gels, lotions, creams, pads, masks, cleansers Local skin irritation; may bleach hair or clothing ```

Answer 35

Topical antimicrobial for acne ``` Twice daily Once daily ( 1% gel, lotion, pledget, solution, foam Rare risk of pseudomembranous colitis ```

Answer 36

Topical antimicrobial for acne Twice daily 2% gel, solution, pledget oral antibiotic 500 mg twice daily (base) Gastrointestinal distress

Answer 37

Topical antimicrobial for acne Twice daily 20% cream, 15% gel Local skin irritation • a dicarboxylic acid , a white powder found in wheat, rye and barley where it is involved in the plant defense response to an infection • it kills acne bacteria and decreases the production of keratin • it is used to treat mild to moderate acne, and also treats post inflammatory hyperpigmentation

Answer 38

``` Oral antibiotic for acne 500 mg twice daily Photosensitivity, gastrointestinal distress; contraindicated in pregnancy and young children ```

Answer 39

``` Oral antibiotic for acne 50 to 100 mg twice daily or 150 mg once daily Photosensitivity, gastrointestinal distress; contraindicated in pregnancy and young children ```

Answer 40

Oral antibiotic for acne ``` 50 to 100 mg twice daily or 1 mg/kd/day of extended release formulation (round to nearest available strength: 45, 65, 90, or 135 mg tablets) Dizziness, drug induced lupus, skin discoloration; contraindicated in pregnancy and young children ```

Answer 41

oral antibiotic for acne Intermittent dosing due to long drug half life; optimum regimen unknown Gastrointestinal distress

Answer 42

oral antibiotic for acne ``` 160 mg/800 mg once to twice daily Stevens Johnson syndrome, toxic epidermal necrolysis ```

Answer 43

Once daily Nausea, breast tenderness, weight gain, thromboembolic events

Answer 44

``` 25 to 200 mg/day in one or two equally divided doses; doses of 50 to 100 mg/day may be as effective as higher doses and reduce side effects especially useful for adult women with menstrual cycle related breakouts of acne on lower face, etc.; some dermatologists combine with oral contraceptives Contraindicated in pregnancy; menstrual irregularity, breast tenderness, minor gastrointestinal symptoms, orthostatic hypotension, hyperkalemia, dizziness, headaches, fatigue ```

Answer 45

``` 0.5 mg/kg/day, increasing to 1 mg/kg/day in one or two equally divided doses; total dose 120 to 150 mg/kg over 20 weeks Teratogenicity (absolutely contraindicated in pregnancy), mucocutaneous effects, hypertriglyceridemia, others ```

Answer 46

Emollients and Corticosteroids for initial choice for mild to moderate psoriasis Topical Vitamin D analogs Calcipotriene and calcitriol to reduce the keratinocyte proliferation tar Tazarotene (retinoid gel) Calcineurin inhibitors (tacrolimus, pimecrolimus) Anthralin Salt water bath

Answer 47

photochemotherapy (PUVA) … uses UVA radiation (under strict medical supervision), which penetrates deeper into the skin without causing sunburn • patients typically ingest the plant photosensitizer psoralen ~ 2 hrs before treatment ~ 3X/week until remission; mechanism unknown • must be protected from sun exposure • increases risk of melanoma

Answer 48

``` for psoriasis inhibits phosphodiest erase 4 (PDE4) specific for cyclic adenosine monophosph ate ( cAMP )   cAMP levels in cells  regulates numerous inflammatory mediators…   nitric oxide synthase, TNF α, IL 23   IL 10 • moderate to severe plaque psoriasis • active psoriatic arthritis • LIBERATE trial shows ~55% patients have ≥ 75% reduction in Psoriasis Area and Severity Index (PASI)… comparable to etanercept  administered orally , well absorbed  hepatic metabolism, primarily CYP3A4  half life of 6 9 hrs  pills ~$70 ea  severe diarrhea, nausea and vomiting possible; weight loss  headache most common CNS complaint, but depression, suicidal ideation, mood changes have been observed ```

Answer 49

PDE4 inhibitor for topical therapy of dermatitis

Answer 50

```  human monoclonal antibody, targets proinflammatory cytokines IL 12 and IL 23  blunts IL 12/IL 23 effects, so :   natural killer cell activation   CD4+ T cell differentiation and activation   MCP 1, TNF α , CXCL 10, IL 8 expression  plaque psoriasis  psoriatic arthritis  Crohn disease  given subQ at 8 12 week intervals following induction at 0 and 4 wks  •>$13k/dose  generally well tolerated, but increases risk for infections  may increase risk for squamous cell carcinomas  hypersensitivity reactions ```

Answer 51

``` human monoclonal antibody, targets proinflammatory cytokine interleukin 17A  blunts IL 17A effects, thereby decreasing its ability to induce the production of many other proinflammatory signaling molecules:   cytokines IL 6, GC CSF, IL 1 β , TGF β , TNF α   chemokines IL 8, GRO α abd NCP 1   prostaglandins  ankylosing spondylitis  plaque psoriasis  psoriatic arthritis  administered subcutaneously… typically 150 mg at weeks 0, 1, 2, 3,and 4 and then every 4 weeks thereafter  may need 300 mg/dose for severe plaque psoriasis  •>$3k/150 mg  generally well tolerated, but increases risk for infections  may causes exacerbations of inflammatory bowel disease  hypersensitivity reactions ```

Answer 52

a humanized monoclonal | antibody against iL 17A with similar indications similar to secukinumab

Answer 53

Liquid nitrogen cryotherapy • Surgical therapy • Pharmacotherapy – Topical 5 fluorouracil (see – Imiquimod … a topical immune response modifier that stimulates local cytokine induction, is an effective therapy – Ingenol mebutate …a substance derived from the sap of the Euphorbia peplus plant, is an effective treatment; has two stages: 1) initial disruption of cell plasma membranes and mitochondria leading to cell necrosis ( chemoablation ) ans 2) neutrophil mediated antibody dependent cellular cytotoxicity that eliminates remaining tumor cells – Topical diclofenac … an NSAID, benefits suggest PG’s may be important for skin carcinogeneis – Retinoids … (discussed • Photodynamic (Red Light) therapy : LED emits strong 635 nm light • Dermabrasion : surgical skin planing • Chemical peels : e.g., with trichloroacetic acid

Answer 54

inhibits thymidylate synthetase , a critical enzyme in the synthesis of DNA • the lack of DNA synthesis in fast growing dysplastic cells prevents cell proliferation and causes cell death • has been used with good success in patients with multiple AKs; effective in >90% who can tolerate it and also treats undectable AKs • causes inflammation and destruction of the lesions (see next slide) rash looking inflammatory response • after 4 6 weeks skin will have progressed from erythema through blistering, necrosis with erosion, and then re epithelialization

Answer 55

``` • surgical removal/ablation: – curettage and electrodessication – Mohs micrographic surgery – X ray radiation – cryosurgery – photodynamic therapy – laser surgery • topical medications: – imiquimod – 5 fluorouracil • advanced BCC – vismodegib or sonidegib : both oral “hedgehog” signaling pathway inhibitors ```

Answer 56

chronic, relapsing immune mediated inflammatory disorder affecting hair follicles resulting in non scarring hair loss – disorder ranges from small patches of alopecia on any hair bearing area to the complete loss of scalp, eyebrow, eyelash, and body hair – u ntreated, ~50% will grow hair back in < 1 year, but recurrence is likely – intralesional or topical corticosteroids – topical immunotherapy … contact allergen such as diphenylcyclopropenone ( is used to cause contact dermatitis, which causes hair growth for unknown reason

Answer 57

– minoxidil : • vasodilates due to K channel opening • promotes hair growth by increasing the duration of anagen (growth phase), shortening telogen (rest phase), and enlarging miniaturized follicles – finasteride • oral inhibitor of dihydrotestosterone (DHT) production, can cause sexual dysfunction • use increases hair count – s urgery … transplantation of hair follicle units (natural groupings of ~ 4 hairs) from regions resistant to hair loss into regions of hair loss

Answer 58

– minoxidil (first line)line): • vasodilates due to K channel opening • promotes hair growth by increasing the duration of anagen (growth phase), shortening telogen (rest phase ), and enlarging miniaturized follicles – anti androgens (second line when minoxidil fails) • spironolactone (androgen partial • finasteride (blocks dihydrotestosterone synthesis) • f lutamide (androgen

Derm drugs Flashcards

(82 cards)